Pharmacodynamics Antihistamine and anticholinergic activity Benzatropine is a
centrally acting anticholinergic and
antihistamine. In terms of its anticholinergic activity, it is specifically an
antimuscarinic and acts a
selective muscarinic acetylcholine M1 and
M3 receptor antagonist. Benzatropine partially blocks cholinergic activity in the
basal ganglia. Animal studies have indicated that anticholinergic activity of benzatropine is approximately one-half that of atropine, while its antihistamine activity approaches that of
mepyramine. Its anticholinergic effects have been established as therapeutically significant in the management of Parkinsonism. Benzatropine antagonizes the effect of
acetylcholine, decreasing the imbalance between the neurotransmitters acetylcholine and
dopamine, which may improve the symptoms of early Parkinson's disease. Benzatropine has been also identified, by a high throughput screening approach, as a potent differentiating agent for
oligodendrocytes, possibly working through
M1 and
M3 muscarinic receptors. In preclinical models for multiple sclerosis, benzatropine decreased clinical symptoms and enhanced re-myelination.
Atypical dopamine reuptake inhibition In addition to its anticholinergic activity, benztropine has been found to increase the availability of dopamine by blocking its
reuptake and storage in central sites, and as a result, increasing
dopaminergic activity. Benzatropine and
analogues are atypical
dopamine reuptake inhibitors, which might make them useful for people with
akathisia secondary to antipsychotic therapy.
Other actions Benzatropine also acts as a
functional inhibitor of acid sphingomyelinase (FIASMA). ==Society and culture==